Antibacterial oxazolidinone analogues having a N-hydroxyacetyl-substituted seven-membered [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit

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• 作者：Hideyuki Suzuki^a ; ^{hsuzuki@itsuu.or.jp} ; Iwao Utsunomiya^a ; Koichi Shudo^a ; Norio Fukuhara^b ; Tsutomu Iwaki^b ; Tatsuro Yasukata^c
• 关键词：Antibacterial ; Oxazolidinone ; [1 ; 2 ; 5]Triazepane ; [1 ; 2 ; 5]Oxadiazepane
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2013
• 出版时间：May, 2013
• 年：2013
• 卷：63
• 期：Complete
• 页码：811-825
• 全文大小：519 K

文摘

We synthesized a series of oxazolidinone analogues bearing a N-hydroxyacetyl-substituted [1,2,5]triazepane or [1,2,5]oxadiazepane C-ring unit as homologues of an earlier drug candidate, eperezolid. Several of these compounds exhibited potent in?vitro antibacterial activities towards not only Gram-positive, but also Gram-negative and linezolid-resistant pathogens. Compounds 21a and 21b, bearing a thiocarbamate side chain, showed high in?vivo activity against methicillin-resistant Staphylococcus aureus SR3637, together with a promising safety profile in terms of weak inhibition of monoamine oxidase and cytochrome P450 isozymes.